| Autor: |
Jeremy M Sivak, Leo A. Hardegger, Stephen Poor, Elizabeth Fassbender, Keith Jendza, Jason Elliott, Shawn Hanks, Debby Long, Chun Zhang, Fang Liu, Rosemarie Cepeda, Amber Woolfenden, Karl Miranda, Leland Johnson, Powers James J, Malay Ghosh, Donglei Liu, Wendy Lee, Vinayak Hosagrahara, Nello Mainolfi, Christopher M. Adams, Catherine Solovay, Bruce D Jaffee, Nan Ji, Erik Meredith, Fupeng Ma, Karen Anderson, Jean-Claude Bizec, Yubin Qiu, Gerald D. Artman, Peter Tarsa, Yao Peng, Yiqin Zhang, Siyuan Shen, Chang Rao |
| Rok vydání: |
2018 |
| Předmět: |
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| Zdroj: |
Journal of medicinal chemistry. 61(4) |
| ISSN: |
1520-4804 |
| Popis: |
A noninvasive topical ocular therapy for the treatment of neovascular or “wet” age-related macular degeneration would provide a patient administered alternative to the current standard of care, which requires physician administered intravitreal injections. This manuscript describes a novel strategy for the use of in vivo models of choroidal neovascularization (CNV) as the primary means of developing SAR related to efficacy from topical administration. Ultimately, this effort led to the discovery of acrizanib (LHA510), a small-molecule VEGFR-2 inhibitor with potency and efficacy in rodent CNV models, limited systemic exposure after topical ocular administration, multiple formulation options, and an acceptable rabbit ocular PK profile. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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